In the course of searching for the new, potent 5-HT₇ antagonists, a group of 14 new tetrahydro-β-carboline derivatives with tetramethylene linker and different (cyclic imide/amide, benzotriazole) terminals were synthesized and evaluated for 5-HT₇ and 5-HT_1A receptor affinity. Compounds with ftalimide, indolinone and 8-azaspiro[4.5]decane-7,9-dione fragments were among the best 5-HT₇ ligands and they also showed a significant activity for 5-HT_1A receptors. For these selected compounds functional profile for 5-HT₇ receptors was determined in adenylate cyclase assay, and their therapeutic potential was further examined in forced swimming, tail suspension and plus-maze tests. Of the analyzed ligands B1019 displayed antidepressant properties whereas for B991 anxiolytic-like activity was detected.

This study was partially supported by the research grant no. 012/2002 from the Polish Pharmacy and Medicine Development Foundation, given by the POLPHARMA Pharmaceutical Works.

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